The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula:
wherein R
1
represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R
2
represents a group —OR
3
or the like, and R
3
represents a hydrogen atom, C1-C6 alkyl group or the like, or R
1
and —(CH
2
)
n
R
2
may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H):
wherein R
41
is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against
Mycobacterium tuberculosis
, multi-drug-resistant
Mycobacterium tuberculosis
, and atypical acid-fast bacteria.
Disclosed are compounds according to Formula I:
wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity.
Also described herein are methods of antagonizing aspartic protease inhibitors in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound according to Formula I.
Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC
4
receptor antagonistic effect.
Verfahren zur Herstellung von 4-Chlor-2-methyl-5-nitro-phenol
申请人:Wella Aktiengesellschaft
公开号:EP0342532A1
公开(公告)日:1989-11-23
Verfahren zur Herstellung von 4-Chlor-2-methyl-5-nitro-phenol (I)
dadurch gekennzeichnet, daß ein 4-Chlor-2-methyl-phenyl-sulfonat der Formel (II)
worin R einen der Reste Methyl, Ethyl, Trifluormethyl, Phenyl oder Tolyl bedeutet, zunächst in 5-Stellung nitriert wird und sodann das entstandene 4-Chlor-2-methyl-5-nitro-phenylsulfonat durch saure oder alkalische Abspaltung des Sulfonylrestes in die Verbindung der Formel (I) überführt wird. Das Verfahren geht von einem technisch verfügbaren und preiswerten Ausgangsstoff aus und ermöglicht die isomerenreine Herstellung von (I) in sehr guter Ausbeute.
The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula:
wherein R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R2 represents a group -OR3 or the like, and R3 represents a hydrogen atom, C1-C6 alkyl group or the like, or R1 and -(CH2)nR2 may bind to each other together with carbon atoms adjacent thereto through nitrogen atoms so as to form a spiro ring represented by the general formula (H):
wherein R41 is hydrogen, C1-C6 alkyl group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and a typical acid-fast bacteria.